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RASS-Enabled S/P–C and S–N Bond Formation for DEL Synthesis

preprint
submitted on 04.01.2020 and posted on 06.01.2020 by Dillon T. Flood, Xuejing Zhang, Xiang Fu, Zhenxiang Zhao, Shota Asai, Brittany Sanchez, Emily J. Sturgell, Julien C. Vantourout, Paul Richardson, Mark E. Flanagan, David W. Piotrowski, Dominik K Kölmel, Jinqiao Wan, Yong Chang, Zhao Wang, Jason Chen, Phil Baran, Philip Dawson
DNA Encoded Libraries have shown promise as a valuable technology for democratizing the hit discovery process. Although DEL provides relatively inexpensive access to libraries of unprecedented size, their production has been hampered by the idiosyncratic needs of the encoding DNA tag relegating DEL compatible chemistry to dilute aqueous environments. Recently Reversible Adsorption to Solid Support (RASS) has been demonstrated as a promising method to expand DEL reactivity using standard organic synthesis protocols. Here we demonstrate a suite of on-DNA chemistries to incorporate medicinally relevant and C–S, C–P and N–S linkages into DELs, which are underrepresented in the canonical methods.

Funding

NIH GM-118176

NIH 1S10OD025208

NIH UL1 TR002551 TL1 TR002551

Pfizer

History

Email Address of Submitting Author

Dawson@scripps.edu

Institution

Scripps Research

Country

United States

ORCID For Submitting Author

0000-0002-2538-603X

Declaration of Conflict of Interest

No Conflicts

Exports